Design, synthesis and preliminary screening of novel 3-(2-N,N-dimethylaminoethylthio) indole derivatives as potential 5-HT(6) receptor ligands.
J Enzyme Inhib Med Chem
; 23(3): 302-12, 2008 Jun.
Article
em En
| MEDLINE
| ID: mdl-18569332
ABSTRACT
The synthesis and potential 5-hydroxytryptamine(6) receptor (5-HT6R) antagonist activity of a novel series of N-arylsulfonyl-3-(2-N,N-dimethylaminoethylthio) indoles has been reported. The molecular modeling, synthesis and in-vitro radioligand binding data of this series are discussed. The present article describes 37 derivatives of the title series. It was observed that the increased side-chain length with the insertion of a sulfur atom did not lead to the loss of binding affinity of these compounds, although the affinities were reduced. The compounds exhibited moderate affinity and selectivity to human 5-HT6 receptors.
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Antagonistas da Serotonina
/
Receptores de Serotonina
/
Indóis
Idioma:
En
Ano de publicação:
2008
Tipo de documento:
Article